<p>Thiourea and guanidine units are found in
nature, medicine, and materials. Their continued exploration in applications as
diverse as cancer therapy, sensors, and electronics means that their toxicity
is an important consideration. We have systematically synthesised a set of
thiourea compounds and their guanidine analogues, and elucidated
structure-activity relationships in terms of cellular toxicity in three ovarian
cancer cell lines and their cisplatin-resistant sub-lines. We have been able to
use the intrinsic luminescence of iridium complexes to visualise the effect of
both structure alteration and cellular resistance mechanisms. These findings
provide starting points for the development of new drugs and consideration of
safety issues for novel thiourea- and guanidine-based materials.</p>